2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Antifolate

Antifolate

Antifolate

Related Products

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Antifolates agents work by antagonizing (blocking) the actions of folic acid (vitamin B9). Antifolates act specifically during DNA and RNA synthesis, exerting a cytotoxic effect during the S- phase of the cell cycle. Antifolates targeting folate metabolism played a pivotal role in drug treatment of malignant, microbial, parasitic and chronic inflammatory diseases.

Folate (folic acid) cofactors are essential for the synthesis and metabolism of amino acids, consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. Major antifolate enzyme targets and exemplary antifolates that target these enzymes include: dihydrofolate reductase (DHFR), thymidylate synthase (TS), GARFTase and AICARFTase.

Antifolate Related Products (144):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-121207
    Denopterin
    		Inhibitor
    Denopterin is a dihydrofolate reductase (DHFR) inhibitor and an antifolate agent. Denopterin is an antimetabolite that has toxic effects on cells and can be used for cancer.
    Denopterin
  • HY-121927
    Mobiletrex
    Mobiletrex is an anti folate and dihydrofolate reductase inhibitor that can be used in research on rheumatoid arthritis.
    Mobiletrex
  • HY-19095
    TNP-351
    TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
    TNP-351
  • HY-B0806AR
    Proguanil hydrochloride (Standard)
    Proguanil (hydrochloride) (Standard) is the analytical standard of Proguanil (hydrochloride). This product is intended for research and analytical applications. Proguanil hydrochloride, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil hydrochloride (Standard)
  • HY-121256
    Chlorasquin
    		Chemical
    Chlorasquin inhibits thymidylate synthetase with an approximate Ki value of 4.9 μM. Chlorasquin is also a folate antagonist, testing the Methotrexate (HY-14519) effect. Chlorasquin binds tighter to dihydrofolate reductase at alkaline pH than does Methotrexate, which is promising for research of antipsoriatic agents.
    Chlorasquin
  • HY-124350R
    10-Formylfolic acid (Standard)
    		Inhibitor
    10-Formylfolic acid (Standard) is the analytical standard of 10-Formylfolic acid. This product is intended for research and analytical applications. 10-Formylfolic acid is a potent inhibitor of dihydrofolate reductase. 10-Formylfolic acid be used as an early indicator of leukemia.
    10-Formylfolic acid (Standard)
  • HY-10820AS
    Pemetrexed-d5 disodium
    Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed-d<sub>5</sub> disodium
  • HY-10819
    AG2034
    AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED.
    AG2034
  • HY-147699
    FRα-IN-1
    		Chemical
    FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
    FRα-IN-1
  • HY-117791
    (R)-Pralatrexate
    		Control
    (R)-Pralatrexate is the (R)-enantiomer of Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor.
    (R)-Pralatrexate
  • HY-12784S1
    Cycloguanil-d6 nitrate
    Cycloguanil-d6 (Chlorguanide triazine-d6) nitrate is the deuterium labeled Cycloguanil nitrate. Cycloguanil nitrate is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil nitrate blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil nitrate inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil nitrate also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
    Cycloguanil-d<sub>6</sub> nitrate
  • HY-10824A
    Talotrexin monoammonium
    Talotrexin monoammonium is the monoammonium salt form of Talotrexin (HY-10824). Talotrexin monoammonium is an analog of Aminopterin (HY-14518), and is a nonpolyglutamatable classic antifolate. Talotrexin monoammonium is a reduced folate carrier (RFC) specific inhibitor and selectively inhibits RFC transport. Talotrexin monoammonium shows antitumor activity by targeting DHFR to inhibit tumor growth.
    Talotrexin monoammonium
  • HY-183053
    UCP1173
    UCP1173, propargyl-linked antifolate, is an antibacterial agent. UCP1173 inhibits DHFR enzymes, with IC50 values of 0.014 μM for DfrB, 0.19 μM for DfrG, 0.27 μM for DfrA, and 0.091 μM for DfrK. UCP1173 inhibits growth of Staphylococcus aureus clinical isolates carrying dfrA, dfrG, or dfrK resistance genes. UCP1173 can be used for the research of bacterial infections.
    UCP1173
  • HY-122378
    Diopterin
    Diopterin is a folic acid analog that is used in leukemia research.
    Diopterin
  • HY-107981R
    LSN 3213128 (Standard)
    LSN 3213128 (Standard) is the analytical standard of LSN 3213128 (HY-107981). This product is intended for research and analytical applications. LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT) with IC50 of 16 nM. LSN 3213128 exhibits anti-tumor activity.
    LSN 3213128 (Standard)
  • HY-B0806R
    Proguanil (Standard)
    Proguanil (Standard) is the analytical standard of Proguanil. This product is intended for research and analytical applications. Proguanil, an antimalarial proagent, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
    Proguanil (Standard)
  • HY-105934A
    Ketotrexate sodium
    Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases.
    Ketotrexate sodium
  • HY-13664R
    Folinic acid calcium (Standard)
    		Chemical
    Folinic acid (calcium) (Standard) is the analytical standard of Folinic acid (calcium). This product is intended for research and analytical applications. Folinic acid calcium (Leucovorin calcium) is a biological folic acid and is generally administered along with methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity.
    Folinic acid calcium (Standard)
  • HY-103396R
    Trimetrexate glucuronate (Standard)
    		Antagonist
    Trimetrexate (glucuronate) (Standard) is the analytical standard of Trimetrexate (glucuronate). This product is intended for research and analytical applications. Trimetrexate glucuronate (NSC 352122) is a folic acid antagonist. Trimetrexate glucuronate affects DNA and RNA synthesis by inhibiting dihydrofolate reductase and preventing the synthesis of purine nucleotides and thymidylate. Trimetrexate glucuronate has potential antitumour activity and can also be used to inhibit Pneumocystis carinii pneumonia.
    Trimetrexate glucuronate (Standard)
  • HY-126878
    11-Oxahomoaminopterin
    		Chemical
    11-Oxahomoaminopterin shows antifolate activity and inhibits Lactobacillus casei DHFFZ with antimicrobial and antitumor activities.
    11-Oxahomoaminopterin